What are Antimetabolite chemotherapy combination drugs?

Name: Drug Landscape Pharmaceutical Database
Creator: Drug Landscape
Published: 2026-01-01
License: https://creativecommons.org/licenses/by/4.0/

Antimetabolite chemotherapy combination drugs are pharmacologic agents that share a common mechanism (typically targeting Thymidylate synthase). 0 are currently marketed, with 8 more in clinical development.

Antimetabolite chemotherapy combination

0 marketed 7 in Phase 3 1 in Phase 2

This page covers all Antimetabolite chemotherapy combination drugs tracked by Drug Landscape: marketed products and active clinical-stage compounds, targeting Thymidylate synthase, Thymidylate synthase, dihydrofolate reductase (pemetrexed); ribonucleotide reductase, DNA polymerase (gemcitabine), PML-RARA fusion protein (ATRA); DHFR and TPMT (MTX and 6-MP).

Targets

Thymidylate synthase · Thymidylate synthase, dihydrofolate reductase (pemetrexed); ribonucleotide reductase, DNA polymerase (gemcitabine) · PML-RARA fusion protein (ATRA); DHFR and TPMT (MTX and 6-MP) · Thymidylate synthase (via fluorouracil)

Phase 3 pipeline (7)

XELOXA · Spanish Cooperative Group for the Treatment of Digestive Tumours (TTD) · Oncology
XELOXA is a combination chemotherapy regimen that inhibits thymidylate synthase and DNA synthesis to kill rapidly dividing cancer cells.
LV5FU2 · Centre Hospitalier Universitaire de Besancon · Oncology
LV5FU2 is a combination chemotherapy regimen that inhibits thymidylate synthase and DNA synthesis to kill rapidly dividing cancer cells.
TS-1 · National Health Research Institutes, Taiwan · Oncology
TS-1 is an oral combination chemotherapy agent that inhibits thymidylate synthase and enhances fluorouracil activity against cancer cells.
Fluorouracil + folinic acid · Odense University Hospital · Oncology
Fluorouracil inhibits thymidylate synthase to block DNA synthesis, while folinic acid enhances its cytotoxic effect by providing reduced folate cofactors.
Folinic Acid + 5 FU · Pfizer · Oncology
Folinic acid enhances the cytotoxic activity of 5-fluorouracil (5-FU) by stabilizing the ternary complex between 5-FU metabolites and thymidylate synthase, thereby increasing DNA synthesis inhibition and cancer cell death.
Chemotherapy（pemetrexed/gemcitabine） · Shanghai Pulmonary Hospital, Shanghai, China · Oncology
Pemetrexed and gemcitabine are antifolate and nucleoside analogue chemotherapy agents that inhibit DNA synthesis by disrupting folate-dependent enzymes and nucleotide metabolism, respectively.
ATRA plus 6-MP and MTX · Wyeth is now a wholly owned subsidiary of Pfizer · Oncology
This combination uses ATRA to differentiate leukemic cells while 6-MP and MTX provide cytotoxic chemotherapy to eliminate rapidly dividing cancer cells.

Phase 2 pipeline (1)

Adjuvant FL · Asan Medical Center · Oncology
Adjuvant FL is a fluorouracil and leucovorin combination chemotherapy regimen designed to enhance immune response and reduce recurrence in cancer patients.

Patent intelligence

antimetabolite chemotherapy combination patent landscape — aggregated cliff calendar, attackable patents, originator estates